ArticleACS medicinal chemistry letters2026
Amino-Acid-Derived Androgen Receptor Modulators.
Article in ACS medicinal chemistry letters, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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2 authors.
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Abstract
Amino-acid-derived arylpropionamide androgen receptor (AR) modulators, termed EPic AR modulators, have been developed through an efficient 2-3 step synthesis from commercially available enantioenriched amino acid starting materials. This modular route delivers gram-scale quantities of the targets in excellent yield and with high enantiomeric excess (>99% ee), overcoming limitations in the enantioselective preparation of selective androgen receptor modulators (SARMs) and antiandrogens (AAs) while unlocking the previously invariant α-amido heteroatom for structural diversification. Binding assays reveal strong AR affinity for several analogs. Initial validation through cellular reporter assays demonstrates tunable antagonism, with select compounds exhibiting a distinctive biphasic profile: low-efficacy partial agonism at low concentrations that transitions to antagonism at higher doses. These results establish a powerful, operationally simple platform for the rapid generation of stereochemically defined AR modulators, offering new opportunities for next-generation therapeutics in muscle-wasting disorders, oncology supportive care, and androgen-related diseases.
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